Chemical Biology Letters
https://pubs.thesciencein.org/journal/index.php/cbl
<p>Chemical Biology Letters is a peer reviewed journal for publication of research and review articles from Medicinal Chemistry, BioChemistry, Chemical Biology, Drug Development and Drug Delivery related studies.</p>ScienceIn PublishingenChemical Biology Letters2347-9825Synthesis and biological evaluation of Trifluoromethoxyphenyl Indole Carboxamide analogs, ADME and toxicity prediction
https://pubs.thesciencein.org/journal/index.php/cbl/article/view/a660
<p>We report synthesis, ADME profile, and biological evaluation of new analogues as effective Anticancer Agents. Trifluoromethoxyphenyl indole-5-carboxamide analogues (4a-4m) were developed as a class of strong inhibitors of BCR-ABL1 kinase. The compounds (4c, 4e, and 4m) showed good anticancer activity in cancer cell lines such as MCF7, MV411 and K562 with IC50 values of 1.4 µM, 1.7 µM, and 1.1 µM, respectively. In human liver microsomes, these substances likewise displayed a favorable ADME profile, good solubility, and minimal clearance. In an oncology program these analogues offer a promising beginning for the development of BCR-ABL1 kinase inhibitors.</p> <p><em>URN:NBN:sciencein.cbl.2024.v11.660</em> </p>
ArticlesAnticancerMolecular docking studyLeukemiaIndole Carboxamideheterocyclic drugsBaban Mohan MulikNoopur SrivastavaDhananjay Pendharkar
Copyright (c) 2024 ScienceIn Publishing
2024-02-232024-02-2366066010.62110/sciencein.cbl.2024.v11.660Exploring Small-Molecule Inhibitors Targeting MAPK Pathway Components: Focus on ERK, MEK1, and MEK2 Kinases in Cancer Treatment
https://pubs.thesciencein.org/journal/index.php/cbl/article/view/a659
<p>Mitogen-activated protein kinases (MAPKs), also known as extracellular signal regulated kinases (ERKs), are found in numerous signal transduction pathways and are triggered by protein kinase cascades. This article will review the present state of MAPK pathway inhibitors, with an emphasis on the characteristics of tiny molecule blockers of the p38, MEK1, and MEK2 protein kinases. Many of these inhibitors have showed potential in experimental animal models of disease, and they are now being investigated in people for inflammatory and cancer diseases. Clinical trials are currently evaluating targeting a subset of cellular signaling cascades and signaling cascades that control pleiotropic cellular activity. These activities will have far-reaching consequences for the management of a wide range of disorders. The Ras-Raf-MEK-ERK (ERK) pathway, on the other hand, is a clear therapeutic target because it is a common downstream route for a range of critical growth factor tyrosine kinase receptors that are frequently changed or overexpressed in human malignancies. Several new medicines that target this route have been discovered and are currently being tested in clinical studies. BAY 43-9006 is one of the most intriguing new agents. Although it was initially created as a Raf kinase inhibitor, it also has the ability to target Flt-3, c-Kit, and VEGFR-2, which helps to explain its antiproliferative and antiangiogenic characteristics. The ERK signaling system in normal and malignant tissue will be discussed in this paper, with a focus on emerging treatments that target the ERK cascade at the Raf kinase level.</p>
Review ArticlesMEK1MEK2MAPKRas-Raf-MEK-ERKBAY 43-9006cancerTuhin MukherjeeSatyajit MohantyJasleen KaurMayukh DasKrishnendu AdhikaryPrity ChatterjeeRajkumar Maiti
Copyright (c) 2024 ScienceIn Publishing
2024-02-222024-02-2265965910.62110/sciencein.cbl.2024.v11.659Remodeling of membrane lipid homeostasis in azole resistant isolates of Candida albicans
https://pubs.thesciencein.org/journal/index.php/cbl/article/view/a658
<p>Azole resistance mechanisms in <em>Candida albicans</em> infections majorly focus around the alteration of target enzymes, overexpression of efflux pump proteins, and changes in lipid metabolism. Our earlier lipidomic studies have linked changes in cellular lipid compositions to drug susceptibilities and phenotypic defects. This study investigates the relationship between whole cell and membrane lipid profiles in isogenic drug-susceptible and resistant isolates of<em> C. albicans</em>. We have examined the fatty acid and sterol snapshot lipidomics in whole cells, plasma membrane, and lipid rafts. Correlations were discovered between these lipid compositions and the observed drug resistance in <em>C. albicans</em>. Although the correlations drawn from cellular and plasma membrane data corroborate, understanding plasma membrane and suborganellar (rafts in this case) lipid changes may provide better insights into their roles in efflux pump activities and localization, and drug susceptibilities.</p> <p><em>URN:NBN:sciencein.cbl.202<strong>4</strong>.v<strong>11</strong>.<strong>658</strong></em></p>
ArticlesCandida albicansLipidsGas ChromatographyMass SpectrometryAzole ResistanceSana Akhtar UsmaniKhushboo AryaBasharat AliShikha ChandraSaumya ChaturvediNitin BhardwajRajendra PrasadAshutosh Singh
Copyright (c) 2024 ScienceIn Publishing
2024-02-212024-02-2165865810.62110/sciencein.cbl.2024.v11.658Correlation of Thyroid Stimulating hormone and Liver function test in Hypothyroid and Euthyroid subjects
https://pubs.thesciencein.org/journal/index.php/cbl/article/view/a661
<p>The thyroid hormones play an important role in basal metabolic rate, and the liver is important in the metabolism of thyroid hormones, so, these two organs affect functioning of one another. The proper evaluation of hepatic functions (LFTs) in patients with thyroid disorders might be of clinical relevance for undertaking preventive and therapeutic strategies. The study was designed as hospital-based retrospective cross-sectional study conducted in Central Clinical Laboratory of Adesh Institute of Medical Sciences and Research, (AIMSR) Bathinda, a tertiary care teaching hospital in Punjab, India, from a period of Jan 2022 to Dec 2023. Cases included 100 newly diagnosed hypothyroid patients not undergoing any treatment for thyroid dysfunction and controls consisted of 100 euthyroid subjects. Levels of thyroid stimulating hormone (TSH) in cases were significantly high as compared to the controls (r=0.268, p=0.03). Levels of aspartate aminotransferase (AST) (r=0.352, p=0.003) and alanine aminotransferase (ALT) (r=0.27, p=0.006) were also significantly high in cases as compared to controls. Comparison of TSH levels in cases with various liver function tests (LFTs) depicted significant correlation with AST (r=0.334, p=0.001) and ALT (r= 0,399, p=0.001). This study is significantly important for consideration of liver injury due to hypothyroidism. Early detection and treatment can prevent further complications and would be helpful during management of hypothyroid patients.</p> <p><em>URN:NBN:sciencein.cbl.2024.v11.661</em></p>
ArticlesHypothyroidismEuthyroidismThyroid Stimulating hormoneAlanine aminotransferaseAspartate aminotransferaseClinical BiochemistryClinical studiesLiver functionsPremjeet KaurVijay SuriNavpreet Kaur
Copyright (c) 2024 ScienceIn Publishing
2024-02-242024-02-2466166110.62110/sciencein.cbl.2024.v11.661Design, synthesis and biological evaluation of novel sulfamoyl benzamides as allosteric activators of human glucokinase
https://pubs.thesciencein.org/journal/index.php/cbl/article/view/a657
<p>Glucokinase (GK) activators, which target the GK enzyme, are an emerging class of therapeutics with promising effects against diabetes. The objective of this work was to create a new group of sulfamoyl benzamide derivatives with the ability to activate GK and evaluate their effectiveness in treating diabetes. From benzoic acid, several compounds containing sulfamoyl benzamide scaffold were synthesized and evaluated for their ability to activate GK in an in vitro enzymatic experiment. <em>In silico</em> docking analyses were employed to explore how the most suitable arrangements in the allosteric area of the GK enzyme interact during binding. The effectiveness of the identified substances in reducing high blood sugar levels was assessed using the oral glucose tolerance test (OGTT) in healthy rats. This evaluation was based on the results of laboratory tests on enzymes and <em>in silico</em> simulations. One of the most active compounds from the antihyperglycemic assay was then tested for its antidiabetic effects in an induced diabetic rat OGTT assay. The <em>in vitro</em> GK activation was best among compounds 1, 6, and 8 (activation fold: 2.03-2.09). In the OGTT assay (normal rats), compounds 1 and 6 showed promising antihyperglycemic activity. <em>In vivo</em> antidiabetic assay confirmed the consistency with <em>in silico</em> and <em>in vitro</em> outcomes. The newly synthesized derivatives of sulfamoyl benzamide have the potential to be used as a basis for the development of further GK activators that are both safe and efficacious and can be administered orally. These activators may be used as therapeutic agents to treat type 2 diabetes.</p> <p><em>URN:NBN:sciencein.cbl.202<strong>4</strong>.v<strong>11</strong>.<strong>657</strong></em></p>
ArticlesAntidiabetic activityDiabetesGlucokinaseAllosteric GK activatorsSulfamoyl benzamidesPrateek SharmaAnju GoyalAjmer Singh Grewal
Copyright (c) 2024 ScienceIn Publishing
2024-01-112024-01-1165765710.62110/sciencein.cbl.2024.v11.657Synthesis, anticancer activity and molecular docking study of (E)-4-(3,4-Dichlorophenyl)-2-((1,3-diphenyl-1H-pyrazol-4-yl)methylene)-3,4-dihydronaphthalen-1(2H)-one derivatives
https://pubs.thesciencein.org/journal/index.php/cbl/article/view/a656
<p>A novel series of (E)-4-(3,4-Dichlorophenyl)-2-((1,3-diphenyl-1H-pyrazol-4-yl)methylene)-3,4-dihydronaphthalen-1(2H)-one derivatives were synthesized by Claisen-Schmidt condensation of 4-(3,4-dichlorophenyl)-3,4-dihydronaphthalen-1(2H)-one and 1,3-diphenyl-1H-pyrazole-4-carbaldehyde. All the synthesised targets were evaluated for their cytotoxicity against a panel of three cancer cell lines (SiHa, MDA-MB-231 and PANC-1). Among the tested compounds many of them exhibited significant anticancer activity, the compound 8a was found to be the most promising analogue in this series with IC50 values of on tested three cancer cell lines.</p> <p><em>URN:NBN:sciencein.cbl.2024.v11.65<strong>6</strong></em></p>
ArticlesClaisen-Schmidt condensationSertralonepyrazole aldehydeanticancer activityMolecular dockingmedicinal chemistryheterocyclic drugsKudikala SadanandamPrasad PinnojuS.K. ManasaMadderla Sarasija
Copyright (c) 2024 ScienceIn Publishing
2024-01-122024-01-1265665610.62110/sciencein.cbl.2024.v11.656Signaling and molecular pathways implicated in oral cancer: A concise review
https://pubs.thesciencein.org/journal/index.php/cbl/article/view/a652
<p>Oral cancer is the sixth most prevalent type of cancer worldwide and third in India out of the different cancer types identified. Mouth and oral cancers collectively refer to cancers of the buccal cavity, lips, oropharynx, hypopharynx, and larynx. Genetic anomalies, the upregulation of several proteins, the deregulation of tumor-suppressive and oncogenes, and risk factors like alcohol and tobacco consumption are a few examples of the known irregularities that contribute to the development of oral cancer through the accumulation of various carcinogenic substances. Oral cancer is caused and developed by multiple molecular and cellular pathways such as PI3K/AKT/mTOR, Ras-Raf-MEK-ERK pathway, Wnt signaling, NF-κB pathway, Hippo pathway, etc. In addition, various genes including TP53, PTEN, CDKN2A, HRAS, PIK3CA, NOTCH1, IRF6, TP63, etc. are also involved in this malignancy. Therefore, it is crucial to have a deep understanding of these pathways to properly understand the development of oral cancer. This concise review focuses on compiling together various signaling and molecular pathways accountable for oral carcinoma development.</p> <p><em>URN:NBN:sciencein.cbl.202<strong>4</strong>.v<strong>11</strong>.<strong>652</strong></em></p>
Review ArticlesOral CancerMolecular MechanismGenes for cancerPI3K/AKT/mTOR signalingprognostic biomarkerNF-kB pathwaycancer signaling pathwaysMonika KumariBhupender S. ChhikaraPriyamvada SinghBrijesh RathiGeeta Singh
Copyright (c) 2023 ScienceIn Publishing
2023-11-022023-11-0265265210.62110/sciencein.cbl.2024.v11.652Reversal of promoter hypermethylation of CADM1 and SOCS1 by leaf extract of Datura metel in cervical cancer cells
https://pubs.thesciencein.org/journal/index.php/cbl/article/view/a654
<p>Cervical cancer ranks as the second most fatal cancer among women in developing countries, trailing only behind breast cancer. Human Papillomavirus (<em>HPV</em>) infection, among various contributors, stands as a primary cause of cervical cancer. Overexpression of DNA methyltransferase 1 (<em>DNMT1</em>) leads to hypermethylation of Cell Adhesion Molecule 1 (<em>CADM1</em>) and Suppressor of Cytokine Signaling 1 (<em>SOCS1</em>), consequently silencing these tumor suppressor genes (TSGs) epigenetically. In this study, we explored the reversal of aberrant methylation in the squamous cervical cancer cells, SiHa using a concentration of 5 µg/ml of <em>Datura metel </em>ethanol- chloroform (E: C) leaf extract. Treating the cells with the extract for 72 hours and consecutively for six days, the DNA fragmentation study for cell apoptosis was performed. The methylation-specific PCR analyzed the DNA aberrant methylation patterns of these TSGs and their subsequent reversal and fragmentation. The results suggest that the <em>Datura metel</em> leaf extract (E: C) was able to cause DNA fragmentation and also effectively reversed the promoter hypermethylation, leading to the reactivation of <em>CADM1</em> and <em>SOCS1</em>. This was evidenced by the reduction in intensity and visual sharpness of the methylation-specific band and the unmethylation-specific band displayed an increase in width and enhanced luminosity in MS-PCR for both genes. This study marks one of the initial global reports showcasing the potential of E: C leaf extract from <em>Datura metel</em> in reversing hypermethylation and reactivating <em>CADM1</em> and <em>SOCS1</em> genes in cervical cancer cells. Further exploration into the phytochemicals of <em>D. metel</em> leaves that demethylate <em>CADM1</em> and <em>SOCS1</em> could unveil a promising candidate for reactivating suppressed genes in cervical cancer.</p> <p><em>URN:NBN:sciencein.cbl.202<strong>4</strong>.v<strong>11</strong>.<strong>654</strong></em></p>
ArticlesCervical cancerEpigeneticsReversal of Promoter hypermethylationTumor suppressor genesDatura metelCADM1SOCS1Mahek SharanNiraj Kumar JhaSaurabh Kumar JhaAbhimanyu Kumar Jha
Copyright (c) 2024 ScienceIn Publishing
2024-01-022024-01-0265465410.62110/sciencein.cbl.2024.v11.654In-vitro cytotoxic studies of 1-hexylcarbamoyl-5-fluorouracil encapsulated nanogels in BMG-1 cells
https://pubs.thesciencein.org/journal/index.php/cbl/article/view/a655
<p>5-Fluorouracil (5-FU) has become one of the most widely employed antimetabolite chemotherapeutic agents in the treatment of several cancers including brain, colorectal, breast, head and neck, pancreas and stomach cancers. The variability in 5-FU pharmacokinetics makes oral dosing impractical due to low and unpredictable bioavailability. Carmofur or HCFU (1-hexylcarbamoyl-5-fluorouracil) is a lypophilic-masked analogue of 5-FU. We present studies on encapsulation of HCFU into the nanogels synthesized through copolymerization of N-isopropylacrylamide (NIPAAM) and N-vinylpyrrolidone (VP) having hydrophobic core and hydrophilic shell by cross-linking with N, N’methylenebisacrylamide. This enables easy entrapment and retention of HCFU inside the hydrophobic core of the nanoparticles. A comparison of the therapeutic efficacies and cell sustainability of 5-fluorouracil, HCFU, HCFU loaded nanogels and unencapsulated nanogels as studied in BMG-1 Cells, is reported.</p> <p><em>URN:NBN:sciencein.cbl.2024.v11.655</em></p>
ArticlesProdrugNanogel5-FUCytotoxicityBMG-1 CellsSheetal BudhirajaAnita YadavRakesh Kumar SharmaRakesh Kumar Sharma
Copyright (c) 2024 ScienceIn Publishing
2024-01-042024-01-0465565510.62110/sciencein.cbl.2024.v11.655Early manifestation of hyperuricemia and its pathophysiological interface with adiposopathy and metabolic syndrome among young adult: Cross-sectional study
https://pubs.thesciencein.org/journal/index.php/cbl/article/view/a653
<p>The association between serum uric acid (SUA) levels and visceral adipose tissue, subcutaneous adipose tissue, and metabolic syndrome (MetS) in young, healthy subjects warrants scientific investigation. In this cross-sectional research involving 114 subjects, various anthropometric parameters, such as body mass index (BMI), waist circumference (WC), and skinfold measurements were measured. Additionally, fasting blood glucose (FBG), SUA concentrations, lipid profiles, and blood pressure were assessed. Mathematical models estimated body fat percentage (BF), total abdominal fat (TAF), intra-abdominal adipose tissue (IAAT), and subcutaneous adipose tissue (SCAT). SUA concentrations were categorized into quartiles: Q1 ≥3.04 mg/dl, Q2 3.05-3.86 mg/dl, Q3 3.89-4.67 mg/dl, and Q4 4.68-7.87 mg/dl. MetS was delineated using the criteria from the National Cholesterol Education Program Adult Treatment Panel III. Statistical methodologies comprised t-tests, one-way ANOVA, and Pearson's correlation. The incidence rates for MetS, hyperuricemia, and hypertriglyceridemia were 11.4%, 5.26%, and 27.19%, respectively. Abdominal obesity, based on WC, was 19.3%. Males showed a more pronounced increase in IAAT (26.23%) than females (13.20%), leading to a total prevalence of 20.18%. The total SCAT incidence was 21.93%, with females (21.53%) outnumbering males (19.67%). The incidence of elevated FBG was 21.93%, suggesting a pre-diabetic condition. Hypertension rates, represented by systolic and diastolic blood pressures, were 3.51% and 15.79% respectively. Metabolic irregularities escalated with increasing SUA levels. The data indicate that young adults manifesting MetS components often exhibit elevated SUA concentrations, proposing that SUA might be an added MetS factor.</p> <p><em>URN:NBN:sciencein.cbl.202<strong>4</strong>.v1<strong>1</strong>.<strong>653</strong></em></p>
ArticlesBody mass indexCentral obesityhyperuricemiaMetabolic SyndromeShipra DasAnil Baran ChoudhuryHemraj DewanganKoushik BhattacharyaSwaraj Bandhu KeshSulagna DuttaPallav Sengupta
Copyright (c) 2023 ScienceIn Publishing
2023-11-062023-11-0665365310.62110/sciencein.cbl.2024.v11.653Synthesis of Indole-Oxadiazole coupled isoxazole hybrids as potent EGFR targeting anticancer agents
https://pubs.thesciencein.org/journal/index.php/cbl/article/view/a651
<p>The synthesis of new indole-oxadiazole coupled isoxazole hybrids (<strong>6a–o</strong>) synthesized by the Cu(I)-catalyzed reaction of in situ generated nitrile oxides with 3-(3,5-dichloro-4-methoxyphenyl)-5-(1-(prop-2-yn-1-yl)-1H-indol-3-yl)-1,2,4-oxadiazole in good yields have been reported here. The chemical structures of all newly synthesized hybrids were confirmed by <sup>1</sup>H-NMR, <sup>13</sup>C-NMR, and Mass spectra. All synthesized compounds were screened for their <em>in vitro</em> cytotoxicity against two breast cancer cell lines MCF-7 and MDA-MB-231 respectively. All the derivatives were more active against MCF7 than MDA-MB-231 cancer cells and few compounds showed better activity than the standard erlotinib. The ability of more potent compounds to inhibit EGFR tyrosine kinase, one of the key enzymes involved in breast carcinomas was evaluated by in vitro enzymatic assay and it was found that the compound (6g) and (6m) had more inhibitory activity IC<sub>50</sub> values 0.311±0.05 and 0.203±0.03 <em>m</em>M than erlotinib (IC<sub>50</sub>=0.421±0.03<em> m</em>M).</p> <p><em>URN:NBN:sciencein.cbl.2024.v11.651</em></p>
ArticlesCytotoxicityEGFR inhibitory activityIndoleIsoxazole1,2,4-oxadiazolhybrid drugsheterocyclic drugsAbhilasha DubbaShiva Kumar Koppula
Copyright (c) 2023 ScienceIn Publishing
2023-11-012023-11-0165165110.62110/sciencein.cbl.2024.v11.651Synthesis of 1,4-disubstituted-1,2,3-Triazole derivatives for investigation of inhibition and molecular docking studies against Xanthine Oxidase
https://pubs.thesciencein.org/journal/index.php/cbl/article/view/a628
<p>This study evaluates the inhibition effect of new 1,4-disubstituted-1,2,3-triazoles against Xanthine Oxidase supplemented by molecular modelling. Nine compounds of 1,4-disubstituted-1,2,3-triazoles by Sharpless's approach have been synthesized in this report. The structures of the synthesized compounds were characterized using FT-IR, <sup>1</sup>H and <sup>13</sup>C-NMR and Mass spectroscopies Among these synthesized molecules (5-bromothiophen-2-yl)(1-(3-fluorobenzyl)-1H-1,2,3-triazole-4-yl)methanone<strong> (</strong><strong>9f) </strong>and (5-Bromothiophen-2-yl(1-(4-methoxybenzyl)-1H-1,2,3-triazole-4-yl)methanone<strong> (</strong><strong>9h) </strong>showed better activity against Xanthine oxidase (XO) compared to allopurinol. In the light of the XO inhibition results, triazoles having of ketone moiety (<strong>9f-i</strong>) were found to be more active than triazoles of ketone-free (<strong>9a-e</strong>). These results were supported by docking models. The docking calculations of the target XO with nine available compounds showed good binding energies with favourable binding interactions. These findings were particularly evident that <strong>9f</strong> (BE -7.29 kcal/mol) and <strong>9h</strong> (BE -7.59 kcal/mol) are represented encouraging higher inhibition properties towards xanthine oxidase (XO), compared to allopurinol as a reference compound. Significant binding energies and interactions obtained by performing the docking studies are demonstrated, in particular, that the compounds <strong>9f </strong>and<strong> 9h</strong> may be more potential bio compounds than the positive compounds, allopurinol, and febuxostat.</p> <p><em>URN:NBN:sciencein.cbl.2023.v10.628</em> </p>
ArticlesTriazolexanthine oxidasemolecular dockingenzyme inhibitionMustafa Nabeel Mirdan MirdanGuler Yagiz ErdemirSamir Abbas Ali NomaTugba Taskin TokBurhan AtesAliye Altundaş
Copyright (c) 2023 ScienceIn Publishing
2023-09-192023-09-1962862810.62110/sciencein.cbl.2023.v10.628Impact of resistin gene polymorphism on insulin resistance and Type 2 diabetes in Iraqi Babylon province patients
https://pubs.thesciencein.org/journal/index.php/cbl/article/view/a629
<p>Resistin is cysteine-rich polypeptide produced by adipocytes and macrophages. This study aims to assess the role of resistin and its gene polymorphisms (rs-34861192 G>A, NG-023447 C>G) as potential link between obesity and insulin resistance in the development of T2DM. Blood samples were collected from 120 participants (60 control are divided into 30 normal weight and 30 obese without T2DM) and (60 patients of Type 2 dm DM) are divided into 30 normal weight and 30 obese). Resistin and insulin levels were increased significantly in the patients’ group (p<0.05). Gene analysis indicated that rs-34861192 was associated significantly (P<0.01) with T2DM in dominant, recessive, and co-dominant models. The rs-34861192 AA genotype showed a significant difference in normal-weight and obese T2DM compared to control (P<0.001) only. The significant difference of GG genotype in normal-weight patients than control exclusively. In the diabetic patients, mutant genotype (AA) of rs34861192 was associated with circulating resistin level. The expression of retn gene was high. Genotype AA of rs- 34861192 was correlated positively with folding change. Mutant AA of rs-34861192 G>A plays an important role in development of T2DM through its effect on resistin levels in the circulation that considered as a major factor for developing T2DM.</p> <p><em>URN:NBN:sciencein.cbl.2023.v10.<strong>629</strong></em></p>
ArticlesInsulinResistinObesityretn geneSNPsgene expressionType 2 diabetesdiabetes geneticsZaid A. A. Al-Shakarchi Ali Hussein AL-MarzoqiSuhayr Aesa Al-Qaysi
Copyright (c) 2023 ScienceIn Publishing
2023-09-252023-09-2562962910.62110/sciencein.cbl.2023.v10.629Synthesis of novel phthalimide-based piperazine conjugated analogs as anti-malarial agents
https://pubs.thesciencein.org/journal/index.php/cbl/article/view/a627
<p>In the present report, we synthesized twelve novel phthalimide analogs and evaluated for antiplasmodial efficacy on Plasmodium falciparum culture. Two molecules exhibited significant inhibition percentages at 1 µM concentration without any apparent cytotoxicity on HepG2 cells. Inhibitory concentration (IC50) for both the hit compounds 6d and 8a was observed in micromolar range, 1.20 µM and 1.66 µM, respectively. Extensive in silico studies conducted indicate plasmepsin IX as a possible target for inhibitory activity of the reported molecules.</p> <p><em>URN:NBN:sciencein.cbl.2023.v10.627</em></p>
ArticlesPhthalimideAmino acid linkerPiperazinePlasmodium falciparumMolecular dockingMeenakshi BansalSumit KumarBrijesh Rathi
Copyright (c) 2023 ScienceIn Publishing
2023-08-072023-08-0762762710.62110/sciencein.cbl.2023.v10.627Small-molecules against Oxidative stress mediated Neurodegenerative diseases
https://pubs.thesciencein.org/journal/index.php/cbl/article/view/a626
<p>Neurodegenerative diseases, marked by the gradual deterioration of neuronal structure and function, impose a significant burden on global healthcare systems. Oxidative stress, resulting from an imbalance between reactive oxidant production and cellular antioxidant defense, is believed to play a significant role in the development of various neurodegenerative disorders, including Alzheimer's disease, Parkinson's disease, and Huntington's disease. Recently, there has been a growing interest in exploring small compounds as potential therapeutic agents to counteract oxidative stress. In addition to highlighting the potential of small molecules to prevent oxidative stress-mediated neuronal damage, this article provides an overview of the function of oxidative stress in neurodegenerative illnesses. Targeting numerous oxidative stress-related pathways, a number of small molecules, including both natural and synthetic antioxidants, have shown promise for neuroprotective benefits. These substances neutralise reactive oxidants, boost endogenous antioxidant defences, reduce inflammation, alter mitochondrial function, and encourage neurotrophic growth.</p> <p><em>URN:NBN:sciencein.cbl.2023.v10.626</em></p>
Review ArticlesNeurodegenerationNeuroblastomaAlzheimer's diseaseParkinson's diseaseHuntington's diseaseOxidative stressChinmay Pal
Copyright (c) 2023 ScienceIn Publishing
2023-08-012023-08-0162662610.62110/sciencein.cbl.2023.v10.626